化学性质:
规格 | 10mM (in 1mL DMSO) 5mg 25mg |
CAS | 83 |
别名 | N/A |
化学名 | (Z)-N-(4-methyl-3-(1-methyl-7-((6-methylpyridin-3-yl)amino)-2-oxo-1,2-dihydropyrimido[4,5-d]pyrimidin-3(4H)-yl)phenyl)-3-(trifluoromethyl)benzimidic acid |
分子式 | C28H24F3N7O2 |
分子量 | 547.53 |
溶解度 | ≥ 5.48mg/mL in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
IC50:The IC50 of GNF-7is 0.005, 0.001, and 0.008 μM in Colo205, SW620, and TrkC-Ba/F3 cells, respectively.
GNF-7 is the type-II inhibitor of T315I-Bcr-Abl [1]. BCR-ABL, constitutively activated tyrosine kinase, is an oncogene associated with chronic myelogenous leukemia (CML) and some cases ofacute lymphocytic leukemia in humans.
In vitro:GNF-7 showed excellent growth inhibitory activity against some human cancer cells. The IC50 of GNF-7is 0.005, 0.001, and 0.008 μM when tested in Colo205, SW620, and TrkC-Ba/F3 cell line, respectively.GNF-7 showed little effect on HEK293T cells, a normal cell line [1].After treated for 24h (7.5mg/kg QD or 15 mg/kg QD), GNF-7 significantly decreaseddisease burden in mice and prolonged overall survival compared to vehicle-controls [2].
In vivo:In acute myelogenous leukemia and lymphoblastic leukemia models, GNF-7 potently and selectively inhibited NRAS-dependent cells [2]. In theT315I-Bcr-Abl-Ba/F3 cell line bioluminescent xenograft mouse model,oral administration of GNF-7 with 10or20mg/kgexhibited significant efficacy against T315I-Bcr-Abl without appreciable toxicity [1].
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标签:GNF-7
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